Sonidegib diphosphate
Based on 13 publication(s) in Google Scholar
Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.97%
- CAS. Nr.: 1218778-77-8
- Formel: C26H32F3N3O11P2
- Molecular Weight:681.49
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Sonidegib diphosphate
More- Nat Med. 2018 Nov;24(11):1752-1761. [Abstract]
- Free Radic Biol Med. 2026 Aug 16:252:493-508. [Abstract]
- J Genet Genomics. 2018 May 20;45(5):237-246. [Abstract]
- J Pathol. 2025 Nov 6. [Abstract]
- Tissue Cell. 2025 Dec 5:99:103263. [Abstract]
- Tissue Cell. 2024 Nov 28:92:102643. [Abstract]
- Cell Physiol Biochem. 2018;47(4):1352-1364. [Abstract]
- bioRxiv. 2025 Oct 11.
- SSRN. 2025 Jul 25.
- bioRxiv. 2024 Jul 25.
- bioRxiv. 2024 Nov 4:2024.10.08.617155. [Abstract]
- bioRxiv. 2023 Nov 6:2023.11.03.565570. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
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In Vivo Efficacy Study
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IF
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IF
Biologische Aktivität
IC50: 1.3 nM (mSmo), 2.5 nM (hSmo)[1]
The IC50 values for Sonidegib (NVP-LDE225) for the major human CYP450 drug metabolizing enzymes is greater than 10 μM[1]. Sonidegib (LDE225), a small molecule, clinically investigated SMO inhibitor, used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34+ chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). Sonidegib interacts directly with SMO, in a similar fashion to cyclopamine, to reduce expression of downstream Hh signaling targets. Primary CD34+ CP-CML cells are cultured in serum free media (SFM)±Sonidegib for 6, 24 and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is significantly downregulated following exposure to Sonidegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1218778-77-8
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Appearance Solid
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Molecular Weight 681.49
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Formel C26H32F3N3O11P2
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Color White to off-white
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SMILES
O=C(C1=C(C)C(C(C=C2)=CC=C2OC(F)(F)F)=CC=C1)NC3=CC=C(N=C3)N4C[C@@H](C)O[C@@H](C)C4.O=P(O)(O)O.O=P(O)(O)O
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Synonyms
Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Med
2018 Nov;24(11):1752-1761. PMID: 30349086 -
Free Radic Biol Med
Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]2026 Aug 16:252:493-508. PMID: 42061481 -
J Genet Genomics
Reduced Smoothened level rescues Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. [Abstract]2018 May 20;45(5):237-246. PMID: 29807798
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Genet Genomics. 2018 May 20;45(5):237-246. [Abstract]
Drug-feeding scheme (upper panel). Memory rescuing effects through treatment with LDE225 (LDE) or Vismodegib (VIS) at 20 mg/kg for 7.5-m-old and 15-m-old mice (lower panel, n=7 for each group).
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J Pathol
Transcriptomic profiling reveals the role of Hedgehog signaling as a biomarker and in the pathogenesis of Ménétrier's disease. [Abstract]2025 Nov 6. PMID: 41199529
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed Sonidegib or DMSO treatment did not affect the weight of mice.
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed immunoblotting with anti-GLI1 and anti-beta-actin antibodies showed GLI1 expression is decreased by the sonidegib treatment, confirming the effective inhibition of Hh signaling. Bar graph represents quantification of the immunoblotting.
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed Hematoxylin and eosin (H&E) stains reveal that Hh inhibitor sonidegib treatment partially rescues the phenotypes in MT-TGFα mice.
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed H+/K+ ATPase positive parietal cells and GIF positive chief cells are significantly increased following sonidegib treatment. UEA1 positive foveolar cells are significantly decreased while GSII positive neck cells show a decreasing trend although the result is not statistically significant. The Ki-67 positive proliferating cells are significantly decreased after sonidegib treatment in stomach tissues.
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Immunofluorescentstaining shows GLI1 expression is decreased following Sonidegib (50 μM; 48 h) treatment whereas pEGFR expression is not changing in gastric organoids from MD patients.
Sonidegib diphosphate purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]
Immunoblotting with anti-pEGFR, anti-GLI1, and anti-b-actin antibodies show GLI1 expression is significantly decreased in the Sonidegib (50 μM; 48 h) treatment group whereas pEGFR expression is not changing in gastric organoids from MD patients. Bar graphs represent quantification of the immunoblotting.
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Tissue Cell
2025 Dec 5:99:103263. PMID: 41365188 -
Tissue Cell
The Shh-p38-NFATc1 signaling pathway is essential for osteoclastogenesis during tooth eruption. [Abstract]2024 Nov 28:92:102643. PMID: 39612595 -
Cell Physiol Biochem
2018;47(4):1352-1364. PMID: 29929201 -
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bioRxiv
2024 Nov 4:2024.10.08.617155. PMID: 39415993 -
bioRxiv
Transcriptomic Profiling Reveals Claudin 18.2 as a Diagnostic Biomarker of Ménétrier's Disease and the Role of Hedgehog Signaling in Pathogenesis. [Abstract]2023 Nov 6:2023.11.03.565570. PMID: 37986961 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (146.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.25 mg/mL (0.37 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (7.34 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
CD34+ CP-CML cells are seeded in SFM alone±Sonidegib±Nilotinib and cultured for 24-72 h prior to assessment. Proliferation is measured using colorimetric assessment of BrDU incorporation. Proportion of viable cells versus those in early and late apoptosis is assessed by flow cytometry using annexin V-FITC and 7-amino-actinomycin D (7-AAD, Via-Probe solution). Cell cycle status is assessed using Ki67 (FITC) expression and 7-AAD incorporation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
The transgenic EGFP+/SCLtTA/TRE-BCR-ABL mouse model is used to investigate the effect of Sonidegib treatment on CML LSC in vivo. Scl-tTa-BCR-ABL mice in the FVB/N background are crossed with transgenic GFP-expressing mice. Bone marrow cells are obtained 4 weeks post induction, GFP+ cells are selected by flow cytometry and transplanted by tail vein injection (106 cells/mouse) into wild-type FVB/N recipient mice, irradiated at 900 cGy, generating a large cohort of mice with similar time of onset of leukemia. Blood samples obtained 4 weeks post transplantation confirmed a neutrophilic leukocytosis in recipient mice. Mice are treated with Nilotinib (50 mg/kg by gavage, daily), Sonidegib (80 mg/kg by gavage, daily), Sonidegib+Nilotinib, or with vehicle alone (control). After 3 weeks of treatment, animals are euthanised and marrow content of femurs and tibiae, spleen cells and blood obtained. Total white cell count (WCC), GFP-expressing WCC, myeloid cells, and GFP+ progenitors and stem cells are measured by flow cytometry. Survival is assessed in a subset of mice for 120d post discontinuation of treatment. Spleen and BM cells from a subset of mice in each arm are pooled and 5×106 cells/mouse (8 mice/condition) are transplanted into wild-type FVB/N recipient mice irradiated at 900 cGy. Engraftment is monitored by drawing peripheral blood (PB) every 4 weeks. The percentage of GFP+ cells in PB is analyzed by flow cytometry.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4. [Content Brief]
[2]. Irvine DA, et al. Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia. Sci Rep. 2016 May 9;6:25476. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4674 mL | 7.3369 mL | 14.6737 mL | 36.6843 mL |
| 5 mM | 0.2935 mL | 1.4674 mL | 2.9347 mL | 7.3369 mL | |
| 10 mM | 0.1467 mL | 0.7337 mL | 1.4674 mL | 3.6684 mL | |
| 15 mM | 0.0978 mL | 0.4891 mL | 0.9782 mL | 2.4456 mL | |
| 20 mM | 0.0734 mL | 0.3668 mL | 0.7337 mL | 1.8342 mL | |
| 25 mM | 0.0587 mL | 0.2935 mL | 0.5869 mL | 1.4674 mL | |
| 30 mM | 0.0489 mL | 0.2446 mL | 0.4891 mL | 1.2228 mL | |
| 40 mM | 0.0367 mL | 0.1834 mL | 0.3668 mL | 0.9171 mL | |
| 50 mM | 0.0293 mL | 0.1467 mL | 0.2935 mL | 0.7337 mL | |
| 60 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6114 mL | |
| 80 mM | 0.0183 mL | 0.0917 mL | 0.1834 mL | 0.4586 mL | |
| 100 mM | 0.0147 mL | 0.0734 mL | 0.1467 mL | 0.3668 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Sonidegib diphosphate Related Classifications
HY-16582 Related Classifications
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